Abstract: The present invention relates to novel pyridazines according to formula (I) processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment and/or prevention of diseases and disorders mediated by Autotaxin.
Type:
Grant
Filed:
October 25, 2019
Date of Patent:
August 31, 2021
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Gerald Juergen Roth, Tom Bretschneider, Christian Andreas Kuttruff
Abstract: The present disclosure relates to various solid state forms of 5-{[(2S,5R)-2,5-dimethyl-4-(tetrahydro-2H-pyran-4-ylmethyl)piperazin-1-yl]carbonyl}-N-(5-fluoro-2-methylpyrimidin-4-yl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-amine and methods of making the same. Such forms of 5-{[(2S,5R)-2,5-dimethyl-4-(tetrahydro-2H-pyran-4-ylmethyl)piperazin-1-yl]carbonyl}-N-(5-fluoro-2-methylpyrimidin-4-yl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-amine are useful in preparation of pharmaceutical compositions and dosage forms for the treatment of cancer, immune disorders and inflammation.
Abstract: The invention provides a method for producing a crystal of a uracil compound with high purity by a process which can be carried out in an industrial scale. Specifically, the invention provides a method for producing a crystal of a uracil compound, wherein the method involves dissolving a composition containing a uracil compound represented by formula (1) in organic solvents consisting of a C3-C6 alcohol solvent and an aromatic solvent to obtain a solution, and precipitating a crystal of said uracil compound from the solution.
Abstract: In various embodiments novel allosteric antagonists of the CRFR1 receptor are provided. It discovered that allosteric CRFR1 receptor antagonists are effective to modulate p-Tau levels in Alzheimer's disease (AD) models. In one illustrative embodiment, a compound that is a CRFR1 receptor antagonist is a compound according to the formula or a pharmaceutically acceptable salt, ester, amide, solvate, or prodrug thereof.
Type:
Grant
Filed:
September 6, 2017
Date of Patent:
August 3, 2021
Assignee:
The Regents of the University of California
Inventors:
Mohammad Parvez Alam, Varghese John, Barbara Jagodzinska
Abstract: The present invention relates to tetrahydroquinoline derivatives of the present invention or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the P2X7 receptor.
Abstract: The instant invention provides pharmaceutical formulations for a long acting injectable drug product comprising a suspension of doravirine for parenteral administration via intramuscular or subcutaneous routes. The drug product can be used for the treatment or prophylaxis of infection by HIV or for the treatment, prophylaxis, or delay in the onset of AIDS (acquired immunodeficiency syndrome) or ARC (AIDS related complex).
Inventors:
Sachin Mittal, Irina Kazakevich, Himanshu Bhattacharjee, Peter Bakker, Luke Schenck, David J. Goldfarb, Amitava Mitra, Donna Carroll, Nazia Khawaja
Abstract: The invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I.
Type:
Grant
Filed:
March 2, 2020
Date of Patent:
August 3, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Elizabeth M. Bacon, Elbert Chin, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, John O. Link, Nathan Shapiro, Teresa Alejandra Trejo Martin, Zheng-Yu Yang
Abstract: The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.
Type:
Grant
Filed:
September 12, 2019
Date of Patent:
July 27, 2021
Assignee:
Novartis AG
Inventors:
Christopher Becker, Xiaolin Li, Peichao Lu, Naomi Samadara Rajapaksa, David Charles Tully, Xiaojing Michael Wang, Qian Zhao
Abstract: Histone deacetylase (“HDAC”)-selective inhibitors covalently bonded to a linker covalently bonded to an E3 ubiquitin ligase ligand, and salts thereof; pharmaceutical compositions containing them; methods of using the composition to inhibit neoplastic cell growth in mammals, including humans.
Type:
Grant
Filed:
February 25, 2020
Date of Patent:
July 13, 2021
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Weiping Tang, Ka Yang, Hao Wu, Zhongrui Zhang
Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.
Type:
Grant
Filed:
March 29, 2019
Date of Patent:
July 13, 2021
Assignee:
Board of Regents, The University of Texas System
Inventors:
Kang Le, Michael J. Soth, Philip Jones, Jason Bryant Cross, Christopher L. Carroll, Timothy Joseph McAfoos, Pijus Kumar Mandal
Abstract: Disclosed embodiments concern kinase inhibitors, such as interleukin receptor associated kinases (IRAK) inhibitors according to Formula 1, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent a kinase-associated disease or condition, particularly an IRAK-associated disease or condition.
Abstract: The present invention provides for the dasatinib-thymine co-crystal and dasatinib-adenine co-crystal. The present invention further provides dasatinib-butanediol solvate. The present invention further provides for crystalline dasatinib-(±)-1, 2-Butanediol, crystalline dasatinib (R)-1, 2-Butanediol, crystalline dasatinib (S)-1, 2-Butanediol and crystalline dasatinib (±)-2, 3-Butanediol and processes for preparation thereof. The present invention also provides for a process for preparation of amorphous dasatinib using dasatinib-butanediol solvate. The present invention further provides for the preparation of anhydrous dasatinib. The present invention also provides for a process for preparation of dasatinib monohydrate from anhydrous dasatinib.
Abstract: A pyrimidine derivative compound of Chemical Formula 1, an optical isomer thereof, or a pharmaceutically acceptable salt thereof, and a composition for preventing or treating cancer comprising the same as an active ingredient. The pyrimidine derivative compound of Chemical Formula 1, the optical isomer thereof, or the pharmaceutically acceptable salt thereof has an excellent selective inhibitory effect especially against TYRO 3 among TAM receptor inhibitory effects, and thus can be used as an excellent composition of preventing or treating cancer without adverse effects resulting from the inhibition of Axl and Mer.
Type:
Grant
Filed:
May 2, 2018
Date of Patent:
July 6, 2021
Assignee:
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
Inventors:
Sung Yun Cho, Chang Hoon Lee, Yong Ki Min, Jong Yeon Hwang
Abstract: Surface-modified nanoparticles are produced by associating ligand interactive agents with the surface of a nanoparticle. The ligand interactive agents are bound to surface modifying ligands that are tailored to impart particular solubility and/or compatibility properties. The ligand interactive agents are crosslinked via a linking/crosslinking agent. The linking/crosslinking agent may provide a binding site for binding the surface modifying ligands to the ligand interactive agents.
Abstract: Disclosed herein are certain 2-oxoquinazoline derivatives of Formula (IA): that are methionine adenosyltransferase 2A (MAT2A) inhibitors. Also disclosed are pharmaceutical compositions comprising such compounds and methods of treating diseases treatable by inhibition of MAT2A such as cancer, including cancers characterized by reduced or absence of methylthioadenosine phosphorylase (MTAP) activity.
Type:
Grant
Filed:
February 12, 2021
Date of Patent:
June 29, 2021
Assignee:
IDEAYA BIOSCIENCES, INC.
Inventors:
Muzaffar Alam, Leah Cleary, Melissa Fleury, Zhonghua Pei, Richard Steel, James Sutton, John E. Knox, Zachary E. R. Newby
Abstract: Disclosed are compounds according to Formula (I), and related pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (I).
Type:
Grant
Filed:
May 18, 2020
Date of Patent:
June 29, 2021
Assignee:
Goldfinch Bio, Inc.
Inventors:
Mark W. Ledeboer, Matthew H. Daniels, Maolin Yu, Jean-Christophe P. Harmange
Abstract: The present invention relates to fused heterocyclic derivatives, processes for their preparation and their use in medicine. Specifically, the present invention relates to a novel derivative represented by the formula (I?), or its pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the derivative or its pharmaceutically acceptable salt thereof, and the method for preparing the derivative and its pharmaceutically acceptable salt thereof. The present invention also relates to the use of the derivative and its pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the derivative and its pharmaceutically acceptable salt thereof in the preparation of medicines, in particularly as IDO inhibitor medicines, for treating and/or preventing cancers. Wherein each substituent of the formula (I?) is the same as defined in the specification.
Abstract: Histone deacetylase (“HDAC”)-selective inhibitors covalently bonded to a linker covalently bonded to an E3 ubiquitin ligase ligand, and salts thereof; pharmaceutical compositions containing them; methods of using the composition to inhibit neoplastic cell growth in mammals, including humans.
Abstract: Provided herein is a process for preparing a pyridazine amine compound of formula V, and a process for preparing dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof. Further, provided herein are novel dichloropyridazine amine compounds of formula IVa, IVb, and mixtures thereof, wherein the amino group is an ethylamino group.
Type:
Grant
Filed:
December 31, 2019
Date of Patent:
June 29, 2021
Assignee:
BASF SE
Inventors:
Eric George Klauber, Michael Rack, Roland Goetz, Sebastian Soergel
Abstract: Compounds of Formula I that inhibit at least one of the A2A and A2B adenosine receptors, and compositions containing compounds of Formula I and methods for synthesizing compounds of Formula I, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, disorders, and conditions, including cancer- and immune-related disorders that are mediated, at least in part, by the adenosine A2A receptor and/or the adenosine A2B receptor.
Type:
Grant
Filed:
May 3, 2018
Date of Patent:
June 29, 2021
Assignee:
ARCUS BIOSCIENCES, INC.
Inventors:
Manmohan Reddy Leleti, Dillon Harding Miles, Jay Patrick Powers, Brandon Reid Rosen, Ehesan Ul Sharif, Rhiannon Thomas-Tran